DK165903B - PHARMACEUTICAL PREPARATION AGAINST ACNE - Google Patents

Abstract

The invention relates to a composition suitable for the treatment of acne. The composition of the present invention comprises as active ingredient an extract of a plant, more particularly the extract of the rhizoma of wheat grass (Graminis rhizoma) optionally in admixture with the extract of other plants and antibacterial agents. The cosmetical compositions of the present invention quickly make oily greasy acne skin relatively symptom-free, while iritating, allergic or light sensitizing side-effects are not observed.

Description

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This invention relates to a composition for the treatment of the most common type of pathological skin changes, seborrhoea, which is primarily caused by the metabolism, especially the various acne forms (blackheads, philippines).

Seborrhoea is a disease process that results from increased and also qualitatively altered activity of the skin's sebaceous glands, a process that manifests itself in an increased secretion of algae with altered composition. Due to the increased sebum production, the skin becomes greasy and there is parakeratosis and various scales.

However, Seborrhoea is also seen in forms where, in addition to the symptoms mentioned, hyperkeratosis can occur in the hair follicles and a clogging thereof with thickened sebum. This manifestation is called comedone formation and occurs primarily in the facial skin and in the Arnozan triangle.

15 According to most of the current beliefs, the appearance of seborrhoea is related to the endocrine system and bacterial infections are the characteristic sequelae.

Acne is a more or less severe manifestation of seborrhoea that occurs during puberty.

20 In the beginning, the fat-shining comedians are seen. As a special symptom. By the acne form that occurs in adolescents, the commonly occurring bacterial species, Corynebacterium aenes, can be identified. For symptomatic treatment of the changes caused by this bacterial species, a Hungarian patent specification 171,517 discloses a composition for oral administration useful in inactivating strains of Corynebacterium aenes in a lyophilized form. The remedy proposed in the patent is based on active immunity.

In addition, younger patients suffering from various types of acne were previously socially stressed due to the severe and conspicuous facial disfigurement, which is why numerous methods have been developed to cure this disease or at least its symptoms. The milder forms of acne vulgaris respond well to a vegetable, vitamin-rich, low-fat and low-carbohydrate diet 2

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appropriate local treatment. In these cases, the patient is often advised to treat the diseased skin areas with sulfur, ictyol, and, where appropriate, salicylic preparations in ointment or shake blend forums in combination with disinfecting lukewarm wraps. Sulfur-containing compounds, 5 cysteine derivatives, are described, inter alia, in West German Patent Specification Nos. 1,908,574, 1,918,907 and 2,620,850 and in U.S. Pat.

4428933. In addition to the commonly known sulfur-containing compounds and peroxide compounds, the composition of the latter also contains natural substances such as mustard, oatmeal, yeast and egg yolk.

10 In the present text, only preparations for local use will be referred to and not preparations for oral administration.

The effect of most of the acne preparations used locally is that the Corynebacterium aenes present in the comedones prefer anaerobic conditions. Treatment with azo compounds and 15 peroxide-containing preparations results in transient symptom relief. In numerous cases, the compounds that locally provide oxygen-rich environments are combined with an antibacterial agent, often resulting in synergism. Compositions of this kind are based on the assumption that the peroxide inhibits the formation of the extracellular lipase, antibiotics inhibit the proliferation of the lipase-producing bacteria {C. aeries'). Such compositions are described in British Pat.

1,539,771, 2,088,717 and 2,090,135, in U.S. Patent No. 4,446,145, in French Patent No. 2,383,667, in West German Petition No. 2,918,943, and in PCT Application 83/628.

25 Other patents are known, the active ingredient of which is primarily antibiotics. In particular, for the treatment of veins, penicillin and erythromycin are used (British Patent No. 1,587,428, U.S. Patent No. 4,261,962; however, the use of tetracycline, neomycin (British Patent No. 1,054,124), clindamycin, lincomycin 30 and griseofulvin (West German Publication No. 2,557,431, European Patent Application Nos. 52,705 and 52,404).

Finally, creams and ointments, which contain naturally occurring plant extract, have also been produced against the veins.

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drugs, alone or in combination with other active ingredients, especially antibiotics.

The composition disclosed in published European Patent Application No. 41,030 contains the alkaloids of Vincea rosea in combination with an agent for promoting absorption. According to Hungarian patent specification No. 190,813, drugs used as an active ingredient in acne preparations are extracted with fruit spirits. At the same time, the preparation contains sulfur-containing compounds (ictyol).

Using the described compositions, an irritant -10, light-sensitizing and often allergenic effect is often seen. In addition, when using sulfur-containing compounds or powerful peroxide-containing preparations, the skin often peels, which is a source of new infections.

The object of the present invention is the preparation of a composition which may cause the disease image of seborrhoea to disappear which allows the skin healing process to proceed rapidly and which does not cause the known side effects.

The basis of the present invention is the recognition that the oily skin seen in the acne disease picture may soon become symptom-free when a skin soothing composition is used, which at the same time speeds up the secretion, disinfects the skin and eventually normalizes sebum secretion. A cream that unites these effects is unprecedented.

German Publication No. 2,922,467 discloses the use of 25 different oral formulations of plant parts of Agropyron repens, preferably dried and finely divided plant parts, especially the stems and inflorescences, for the treatment of hyperuricemia and hyperlipidemia, and also the possibility of using various extracts of Agropyron repens for oral intake and for the same therapeutic purposes.

From French Patent Specification No. 1,367,618 are known compositions intended for topical treatment of "orange skin", and which include, inter alia, may include 4

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keep constituents extracted from mercury ("chiendent") by a volatile solvent such as ethanol. The entire plant is probably used, as there is no indication of use of one or more specified parts of the plant.

5 Surprisingly, it has now been found that common mercury (Agropyron repens) contains in its root (Graminis rhizoma) substances which - when extracted with water - and the extract is formulated together with at least the carrier commonly used in the cosmetic industry - and Adjuvants - Can be used to successfully treat the various acne forms.

The present invention thus relates to a pharmaceutical composition for topical use against the various forms of acne, in particular in the form of creams, tonics, soaps, body lotions, face packs and shampoos, characterized in that it contains from 15 to 95% by weight of a biologically active aqueous extract of rootstock (Graminis rhizoma) from common mercury (Agropyron repens) and 5-98% by weight of the additives and / or diluents commonly used in cosmetics, preferably natural fats, oils, emulsifiers, preservatives, fragrances and possibly 20 antibodies active agents, and possibly other plant extracts.

The normalizing effect exerted on the skin can be attributed to the content of inositol, triticin, saponin, carotene, silicic acid, malic acid, citric acid, tannins, vitamins and carbohydrate.

The preparation does not dry out or irritate the skin.

The beneficial effects of the Graminis rhizoma extract are attributed to the fact that the extract contains a relatively high amount of saponin, which at low doses stimulates the secretion and promotes the resorption of other substances. However, the saponin content of the compositions may be increased by further adding saponin-containing drugs to the extract (e.g. Equiseti herba),

As can be seen from the above, compositions of the invention can be used to combat the bacterial accompanying various acne forms.

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5 rial infection contain antibiotics. These preparations also provide, in the case of more severe forms of acne, a relatively short time. The extract of Graminis rhizoma and the antibiotic complement each other very well.

For example, as an antibiotic, penicillin, erythromycin, oxy-tetracycline or neomycin can be used. Erythromycin is preferred, especially in the form of erythromycin lactobionate.

Among other plant extracts which can be incorporated into a composition of the invention, for example, extracts selected from rosehip, 10 mushroom extract, thyme extract and chamomile extract are suitable.

A composition according to the invention can take different forms, for example, the composition can be formulated as cream, face tonic, soap, body lotion, face milk, shampoo and jelly face packs.

The invention will now be further illustrated by way of example.

Examples 1-13 show the preparation of the plant extracts, and the further examples illustrate the formulation of these extracts for useful compositions.

EXAMPLE 1

Preparation of an aqueous extract of the rootstock (Graminis rhizoma) 20 from common mercury (Agropyron repens) 1 kg of purified and crushed rhizomes is stirred in 100 liters of water at 95 ° C for 2 hours. The mixture is then centrifuged. The extract obtained (ca.

90 kg) are stored so far for use in a cold place where it is protected from light and where air is excluded.

6

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EXAMPLE 2

Preparation of an aqueous extract of the terrestrial shoots (Equiseta herba) from mushrooms (Equisetum arvense L.) 10 kg of purified and finely divided shoots from mushrooms are stirred in 100 liters of water for 20 minutes at 90 ° C. Next, the mixture is filtered. The filtrate is stored protected from heat, light and air for further use.

EXAMPLE 3

Preparation of an alcohol extract of the above ground shoots (Equiseta herba) from mushrooms (Equisetum arvense L.) 10 10 kg of purified and crushed above ground shoots are stirred in 60 liters of 70% ethanol. The mixture is allowed to stand for 5 days with stirring sometimes daily. Next, the mixture is filtered and the filtrate is stored for further use in a cold place where it is protected from light and where air is excluded.

EXAMPLE 4

Preparation of aqueous extract of fake fruit (Cynosbati pseudofruetus) from wild rose (Fosa canina) 1 kg dried and finely divided hips are soaked in 60 ° C hot water for 45 minutes. Next, the mixture is filtered and the filtrate is mixed with a preservative and finally stored protected from heat, light and air until further use.

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EXAMPLE 5 7

Preparation of an alcohol extract of fake fruit (Cynosbati pseu-dofructus) from wild rose (Rosa canina)

The process as well as the amount of plant material used and the volume of 70% ethanol used are as described in Example 3.

EXAMPLE 6

Preparation of an aqueous extract of flowers (Chamomillae floss) from chamomile (Matricaria) 10 kg of dried and purified chamomile flowers are stirred in 80 liters of water at 10 80 ° C for 10 minutes. Next, the mixture is filtered. The filtrate is stored protected from heat, light and air for further use.

EXAMPLE 7

Preparation of an alcohol extract of flowers (Chamomillae flos) from chamomile (Matricaria) 15 According to Ph. Hg. VI, using flowers and 70% ethanol in a weight ratio of 1:10.

EXAMPLE 8

Preparation of an aqueous extract of leaves (Thymi herba) from thyme (Thymus serpyllum L.)

20 10 kg of dried and purified thyme leaves are stirred in 80 liters of water at 90 ° C

for 15 minutes. Next, the mixture is filtered and the filtrate is stored protected from heat, light and air for further use.

8

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EXAMPLE 9

Preparation of an alcohol extract of leaves (Thymi herba) from thyme (Thymus s is py Hum L.)

The process is as described in Ph. Hg. VI, using leaves 5 and 70% ethanol in a weight ratio of 1:10.

EXAMPLE 10

Preparation of aqueous combined drug extract

A mixture of Equiseta herba, Cynosbati pseudofruce tusk and Graminis rhizoma in a ratio of 1: 5: 1.5 is soaked in a sevenfold amount of water 10 at 60 ° C for 3 days. Next, the mixture is filtered and the filtrate is stored protected from heat, light and air for further use.

EXAMPLE 11

Preparation of a combined alcohol-drug extract

A mixture of thyme leaves and chamomile flowers prepared in a ratio of 1: 2.5 is comminuted and soaked in 90% ethanol for 24 hours. The alcohol solution is filtered and stored protected from heat, light and air for further use.

EXAMPLE 12

Preparation of a biologically active substance with 5 components 20 The solutions prepared according to Examples 10 and 11 are mixed in a 1: 1 ratio. The mixture is formulated according to the prior art in the cosmetic industry.

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EXAMPLE 13 9

Preparation of a dry extract of Graminis rhizoma

The aqueous extract of Example 1 is lyophilized under aseptic conditions. The obtained lyophilizate is sealed airtight and 5 is stored protected from heat and light.

EXAMPLE 14 Day Cream

Aqueous extract of Graminis rhizoma according to Example 1 28.0 g

Cetyl alcohol 4.5 g Stearic acid 4.0 g

Brij ™ 721 (polyethylene glycol / stearyl alcohol ether) 4.0 g

Cosmetic Vaseline Oil 1.5 g

Castor oil 2.0 g

Propylene glycol 5.0 g Retinoic acid 0.05g

Ethanol 96% 5.0 g

Distilled water 45.55g

Stabilizer 0.2 g

Perfume 0.2 g Example 15 Cream

Aqueous extract of Graminis rhizoma according to Example 1 28.0 g

Cetyl alcohol 6.5 g

Stearin 5.4 g Cosmetic Vaseline Oil 1.5 g

Propylene glycol 5.0 g

Sorbitol 3.0 g

Sodium lauryl sulfate 0.5 g 10

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Nipagin® M (methyl p-hydroxybenzoate) 0.2 g

Erythromycin (free base) 1.5 g

Ethanol 96% 4.0 g

Distilled water, preservative 44.2 g 5 Perfume 0.2 g EXAMPLE 16 Wash emulsion

Aqueous extract of Graminis rhizoma according to Example 1 28.0 g

Aqueous extract of chamomile flowers of Example 6 2.0 g 10 Aqueous extract of the rose of Example 4 5.0 g

Hostaphat ™ KL 340 N 2.0 g (alkyl polyglycol ether orthophosphoric ester)

Hostacerin® DGS 4.0 g (oxyethyl ether fatty acid polyglycerin ether) Hostacerin® PN 73 0.6 g (sodium salt of acrylic acid / acrylamide copolymer)

Paraffin oil 5.0 g

Isopropyl palmitate 6.0 g

Propylene glycol 3.0 g 20 Distilled water, preservative 44.2 g

Perfume 0.2 g Example 17 Soap Dry extract of Graminis rhizoma according to Example 13 2.0 g 25 Soap Chips 60.0 g

Hostapon ™ CT 10 ', 0 g (palm kernel fatty acid methyl tauride Na salt)

Sodium polyphosphate 10.0 g

Sodium citrate 13.0 g 11

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EXAMPLE 18 Liquid Soap

Aqueous extract of Graminis rhizoma according to Example 1 30.0 g

Aqueous extract of mushrooms according to Example 2 2.0 g 5 Aqueous extract of the hips according to Example 4 5.0 g

Genapol® TSM (alkyl ether sulfate in non-ionic dispersion) 3.0 g

Genapol® LRO 35.0 g (alkyl diglycol ether sulfate Na salt and fatty alcohol)

Medilan * KA (Neutralized Palm Nucleic Acid Carcoside) 8.0 g 10 Sodium Chloride 1.3 g

Distilled water, preservative 15.5 g

Perfume 0.2 g EXAMPLE 19 Shampoo 15 Aqueous extract of Graminis rhizoma of Example 1 24.0 g

Aqueous thyme extract of Example 8 4.0 g

Aqueous extract of the rose hip of Example 4 6.0 g

Aqueous extract of chamomile flowers of Example 6 3.0 g

Genapol® ZRO (alkyl triglycol ether sulfate Na salt) 35.0 g Genapol® AMS 10.0 g (acylaminopolyglycol ether sulfate triethanolamine salt)

Betaine 8.0 g

Coconut fatty acid ethanolamide 2.0 g

Distilled water, preservative 6.4 g Sodium chloride 1.4 g

Perfume 0.2 g EXAMPLE 20

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12

Jelly for face packs

Aqueous extract of Graminis rhizoma according to Example 1 25.0 g

Aqueous extract of mushrooms according to Example 2 10.0 g 5 Aqueous extract of the hips according to Example 4 5.0 g

Carbopol® 940 (carboxyvinyl polymer) 1.0 g

Sodium liquor 10% 2.0 g

Distilled water, preservative 56.8 g

Perfume 0.2 g Example 21

tonic

Aqueous extract of Graminis rhizoma according to Example 1 28.0 g

Erythromycin lactobionate 2.25 g

Propylene glycol 10.0 g Ethanol 96% 43.5 g

Ion Exchanged Water 16.25 g EXAMPLE 22 Day Cream

Aqueous extract of Graminis rhizoma of Example 1 28.0 g 20 Erythromycin lactobionate 2.25 g

Getyl alcohol 10.0 g

Brij ™ 721 4.0 g

Carbopol® 940 0.10 g

Nipagin® M 0.20 g 25 Ion exchanged water 55.45 g

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13

The compositions described in the Examples were subjected to a clinical study. The study included 69 people (43 women, 26 men). The age distribution was between 12 and 30 years, the average age was 16 years. Patients were divided into the following groups severity-5 severity of acne: 55 patients had acne comedonica with severe symptoms, of which 25 had widespread papulopustulosis, and 3 patients had acne conglobata.

The severity of the disease processes, on the basis of the non-inflamed (open and closed comedones) and inflamed (papules, pustules) 10 manifestations found on a cheek were divided into 4 degrees: In fewer than 10 II 11-25 III 26-50. IV more than 50 15 The number of persons treated, the severity of the clinical examination result and the results obtained with the preparations are shown together in Table I (persons who simultaneously had different forms of acne manifestation appear in the table once during each manifestation form). In addition, adverse reactions (burns, itching, skin redness, dandruff) were assessed in the form of subjective and objective complaints.

When treated with the composition of Example 14, patients with severity II and III (for the most part acne comedonica) for a period of 8-12 weeks could be kept symptom-free or at least showed significant improvement. When combining the various acne forms, further continuous treatment was required. Patients who had comedone formation and grade IV papulo pustules had to be treated for longer than 12 weeks.

In 13 patients, a photo-spot test was performed during the co-involvement of control subjects. The mean age of the patients was 13.5 years (12-18 years); there were 2 men and 11 women. 9 of the patients suffered from acne comedonica, 4 of the acne papulopustulosa. The epicutant applied substance was removed after 24 hours. Next, the tested areas became 14

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as well as the corresponding areas (i.e. control areas) irradiated with 5 J / cm 2 light energy for 20 minutes on the opposite side of the body.

It could be stated that neither patients nor control subjects complained of irritant effects, early or late 5 allergic reactions, respectively.

The preparation of Example 21 was tested in 9 patients. Of areas that came to local application were mainly the face, often the back, shoulders and chest. After a thorough cleansing with warm soapy water of the areas to be treated, the 10 skin was smeared, for the first 10 days twice daily, later only once daily. In all cases, an improvement was seen; This one was most noticeable in cases of severe acne. In cases of seborrhoic oily skin, the facial redness took off, the itching became milder and the inflammations disappeared. In more severe cases with papulo pustules, the subjective complaints (burning, itching) often became weaker. With continuous treatment, the number of papules still decreased, the greasy sheen and the comedone formation dimmed.

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Claims (3)

1. Pharmaceutical composition for topical application against the various forms of acne, especially in the form of creams, tonics, soaps, body lotions, face packs and shampoos, 5 characterized in that it contains 2-95% by weight of a biologically active aqueous extract of the rootstock. (Graminis rhizoma) from common mercury (Agropyron repens) and 5-98% by weight of the additives and / or diluents commonly used in cosmetics, preferably natural fats, oils, emulsifiers, preservatives, fragrances and optionally antibacterial agents, and optionally further other plant extracts. Composition according to claim 1, characterized in that it contains as antibacterial agent 0.2-6.0% by weight of antibiotics, preferably erythromycin, especially in the form of erythromycin lactobionate. Composition according to claim 1, characterized in that it contains as an additional plant extract extract of rose, mushroom, thyme and / or chamomile.